TPX-0022

TPX-0022 is an inhibitor of Src, MET, and CSF-1 receptor tyrosine kinase (FMS) kinases (IC50s = 0.12, 0.14, and 0.76 nM, respectively). It inhibits the proliferation of MKN45 and SNU-5 human gastric cancer cells (IC50s = 0.2 and 0.17 nM, respectively), as well as Ba/F3 pro-B cells expressing TEL-CSF1R (IC50 = 19.3 nM). TPX-0022 (100 nM) inhibits cell migration of HCC827 human lung cancer cells. It inhibits tumor growth in an MKN45 mouse xenograft model when administered at doses of 10 and 30 mg/kg. TPX-0022 (10 mg/kg) also inhibits phosphorylation of MET at Tyr1234 and Tyr1349 in the same model.Formal Name: (7S)-3-amino-14-ethyl-11-fluoro-4,5,6,7,13,14-hexahydro-7-methyl-4-oxo-1,15-etheno-1H-pyrazolo[4,3-f][1,4,8,10]benzoxatriazacyclotridecine-12-carbonitrile. CAS Number: 2271119-26-5. Synonyms: CSF1R-IN-2, CSF1R Inhibitor 2, Elzovantinib. Molecular Formula: C20H20FN7O2. Formula Weight: 409.4. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: Ethanol: 5mg/ml. lambdamax: 215, 271 nm. SMILES: CCN(CC1=C(C#N)C(F)=CC=C1O[C@H](CNC2=O)C)C3=NC4=C2C(N)=NN4C=C3. InChi Code: InChI=1S/C20H20FN7O2/c1-3-27-10-13-12(8-22)14(21)4-5-15(13)30-11(2)9-24-20(29)17-18(23)26-28-7-6-16(27)25-19(17)28/h4-7,11H,3,9-10H2,1-2H3,(H2,23,26)(H,24,29)/t11-/m0/s1. InChi Key: UUDPUQDMSHQSKH-NSHDSACASA-N.